| Company Name: |
ShangHai Caerulum Pharma Discovery Co., Ltd.
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| Tel: |
18149758185 |
| Email: |
sales-cpd@caerulumpharma.com |
| Products Intro: |
Product Name:His121 ARG57
CAS:2135785-20-3
Purity:98% Package:10g/;1g/;100mg/;10mg/ Remarks:1g
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| Company Name: |
DC Chemicals
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| Tel: |
021-58447131 13564518121 |
| Email: |
sales@dcchemicals.com |
| Products Intro: |
Product Name:MAGL-IN-4
CAS:2135785-20-3
Purity:98% HPLC Package:100mg，250mg，1g
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| | His121 ARG57 Basic information |
| Product Name: | His121 ARG57 | | Synonyms: | His121 ARG57;MAGL-IN-4;Monoacylglycerol lipase,CB1,lipase,monoacylglycerol,CB2,Inhibitor,inhibit,BBB,barrier,MAGLIN4,MAGL IN 4,blood-brain,endocannabinoid,hERG,FAAH,2-AG,ABHD6,MAGL;7-Oxa-5-azaspiro[3.4]octan-6-one, 2-[[3-[(3-chloro-4-methylphenyl)methoxy]-1-azetidinyl]carbonyl]-, cis- | | CAS: | 2135785-20-3 | | MF: | C18H21ClN2O4 | | MW: | 364.82 | | EINECS: | | | Product Categories: | | | Mol File: | 2135785-20-3.mol |  |
| | His121 ARG57 Chemical Properties |
| Boiling point | 630.7±55.0 °C(Predicted) | | density | 1.38±0.1 g/cm3(Predicted) | | pka | 12.13±0.40(Predicted) |
| | His121 ARG57 Usage And Synthesis |
| Biological Activity | MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 6.2 nM. MAGL-IN-4 can penetrate the blood-brain barrier (BBB). MAGL-IN-4 enhances endocannabinoid signaling mostly by the increase in the level of 2-AG via selective MAGL inhibition in the brain[1].
MAGL-IN-4 (compound 4f) shows a high LLE (5.9), a logD of 2.3 for MAGL[1]. MAGL-IN-4 exhibits no inhibition toward the closely related serine hydrolases (FAAH and ABHD6; all IC50>10000 nM). MAGL-IN-4 has no significant binding potentials to cannabinoid receptors (CB1: 19% and CB2: 5% at 10 μM), and low hERG liability (14.4% inh. at 10 μM, manual patch clamp, without BSA)[1].
MAGL-IN-4 (compound 4f; 0.1-10 mg/kg; oral; single dose) results in a significant elevation in the level of 2-AG and reduction in that of arachidonic acid (AA) from 0.3 mg/kg in C57BL/6J mice[1]. | | References | [1]. Shuhei Ikeda, et al. Design and Synthesis of Novel Spiro Derivatives as Potent and Reversible Monoacylglycerol Lipase (MAGL) Inhibitors: Bioisosteric Transformation from 3-Oxo-3,4-dihydro-2 H-benzo[ b][1,4]oxazin-6-yl Moiety. J Med Chem. 2021 Aug 12;64(15):11014-11044. |
| | His121 ARG57 Preparation Products And Raw materials |
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